Surface-modified solid lipid nanoparticulate formulation for ifosfamide: development and characterization.

ABSTRACT

AIMS: The present research focuses on the development of the surface modified solid lipid nanoparticulate (SLN) system for enhancing the stability and sustaining the release of a model hydrophilic drug ifosfamide. MATERIALS & METHODS: SLNs consisting of glyceryl monooleate (GMO) and chitosan were prepared by double emulsion technique, crosslinked with sodium tripolyphosphate, followed by lyophilization under two different vacuum conditions. The physicochemical characterization of SLNs included evaluation of surface morphology, particle size and surface charge, moisture content and physical state of the drug in the delivery system. The in vitro drug release and the stability were evaluated using high-performance liquid chromatography and liquid chromatography/mass spectrometry, respectively. Cellular permeability and subcellular localization studies were performed using Caco-2 cells. RESULTS: Different chamber pressures during lyophilization produced SLNs with different morphologies and moisture contents. SLNs demonstrated high encapsulation efficiency, sustained release, and enhanced stability of ifosfamide with a high cellular uptake and permeability for Caco-2 cells. CONCLUSION: GMO and chitosan SLNs could be successfully used for enhancing the stability, sustaining the release, enhancing the targeting and permeability characteristics of ifosfamide.